anisotropine methyl bromide | 80-50-2

• 物质功能分类: 天然产物 - 生物碱
• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 托烷生物碱
• 英文名称: anisotropine methyl bromide
• 英文别名: Anisotropin-brommethylat；octatropine methylbromide；[(1R,5R)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octan-3-yl] 2-propylpentanoate;bromide
• CAS: 80-50-2
• 化学式: Br*C₁₇H₃₂NO₂
• 分子量: 362.351
• InChiKey: QSFKGMJOKUZAJM-CTHHTMFSSA-M

物化性质

• 熔点：
  329°
• 溶解度：
  可溶于氯仿（少许）、甲醇（少许）
• 颜色/状态：
  CRYSTALS FROM ACETONE
• 气味：
  PROBABLY ODORLESS
• 味道：
  BITTER TASTE
• 稳定性/保质期：
  STABLE IN LIGHT, HEAT, & AIR.

计算性质

• 辛醇/水分配系数(LogP)：
  0.52
• 重原子数：
  21
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.94
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  3

ADMET

毒理性

• 相互作用

食物减少了大鼠对溴化甲基阿尼索特平的吸收速率，且有证据表明存在可饱和过程，影响这种化合物的肠道吸收。

RATE OF ABSORPTION OF ANISOTROPINE METHYL BROMIDE IS REDUCED BY FOOD IN RAT, & THERE IS EVIDENCE OF SATURABLE PROCESS, INFLUENCING INTESTINAL ABSORPTION OF THIS CMPD.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

...抗胆碱能药物，如阿尼索特罗平...可能会与地高辛发生相互作用.../可能导致血清地高辛水平升高/. /阿尼索特罗平/

...ANTICHOLINERGIC AGENTS, SUCH AS ANISOTROPINE...WOULD BE EXPECTED TO INTERACT WITH DIGOXIN.../MAY CAUSE INCR SERUM DIGOXIN LEVELS/. /ANISOTROPINE/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

地西泮和甲溴氧托品相互作用，在减少离体兔空肠的自发和刺激胃肠动力以及在兔结肠和狗胃袋的体内方面表现积极。

DIAZEPAM & OCTATROPINE METHYLBROMIDE INTERACTED POS IN REDUCING SPONTANEOUS & STIMULATED GI MOTILITY IN ISOLATED RABBIT JEJUNUM & IN VIVO IN RABBIT COLON & DOG GASTRIC POUCH.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

抗胆碱能药物的尿排泄可能会因尿液的碱化而延迟，使用尿液碱化剂如：含钙和/或镁的抗酸剂、碳酸酐酶抑制剂、柠檬酸盐、碳酸氢钠，从而增强抗胆碱能药物的治疗效果和/或副作用。抗胆碱能药物，抗痉挛药。

Urinary excretion of anticholinergics may be delayed by the alkalinization of the urine, /with the use of urinary alkalizers such as: calcium- and/or magnesium-containing antacids, carbonic anhydrase inhibitors, citrates, sodium bicarbonate/ thus potentiating the anticholinergics' therapeutic and/or side effects. /Anticholinergics, antispasmodics/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

...一些在高剂量后出现的副作用是由于神经节阻断。...毒性剂量...产生...抗胆碱能中毒的典型表现，并伴有神经节阻断的附加效应，罕见地，还会出现神经肌肉阻滞，但通常没有显著的中枢神经系统涉及。/季铵化合物/

...SOME OF SIDE EFFECTS SEEN AFTER HIGH DOSES ARE DUE TO GANGLIONIC BLOCKADE. ... TOXIC DOSES...PRODUCE...USUAL MANIFESTATIONS OF ANTIMUSCARINIC POISONING WITH ADDNL EFFECTS OF GANGLIONIC & RARELY, NEUROMUSCULAR BLOCK, BUT USUALLY WITHOUT SIGNIFICANT CNS INVOLVEMENT. /QUATERNARY AMMONIUM CMPD/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

口服给药后吸收差且不稳定...穿透结膜的能力也很差，以至于...这类化合物在眼科学中价值有限。中枢作用通常不足，因为这些药物不易通过血脑屏障。...关于命运和排泄所知甚少.../季铵化合物/

...POORLY & UNRELIABLY ABSORBED AFTER ORAL ADMIN... PENETRATION OF CONJUNCTIVA IS ALSO POOR, SO THAT...CMPD ARE OF LITTLE VALUE IN OPHTHALMOLOGY. CENTRAL EFFECTS ARE GENERALLY LACKING, BECAUSE THESE AGENTS DO NOT READILY PASS BLOOD-BRAIN BARRIER. ...LITTLE...KNOWN OF FATE & EXCRETION... /QUATERNARY AMMONIUM CMPD/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

全身autoradiography小鼠SC，口服，或IP剂量的抗痉挛，[(14)C]莨菪碱甲溴显示，肠道器官（肾脏，肝脏，腮腺和肠）中的主要分布。

WHOLE-BODY AUTORADIOGRAPHY OF MICE GIVEN SC, ORAL, OR IP DOSES OF ANTISPASMODIC, [(14)C]ANISOTROPINE METHBROMIDE SHOWED THAT PARENTERAL DOSES WERE DISTRIBUTED MAINLY IN EXCRETORY ORGANS (KIDNEYS, LIVER, SALIVARY GLANDS, & INTESTINES).

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

一些14C标记的阿尼索托品甲溴盐在给予小鼠后存在于胃粘膜、胰腺、输卵管、子宫和输精管中。这种阳离子不太可能轻易通过生物膜扩散，似乎不会轻易穿过血脑屏障、胎盘屏障或胃肠道上皮。

SOME (14)C /ANISOTROPINE METHBROMIDE/ WAS...PRESENT IN STOMACH MUCOSA, PANCREAS, OVIDUCTS, UTERUS, & SPERMATIC DUCTS /AFTER ADMIN TO MICE/. CATION WOULD NOT BE EXPECTED TO DIFFUSE EASILY ACROSS BIOLOGICAL MEMBRANES...DID NOT APPEAR READILY TO CROSS BLOOD-BRAIN OR PLACENTAL BARRIERS, OR GASTROINTESTINAL EPITHELIUM.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险品标志：
  Xn,N
• 安全说明：
  S36,S60,S61
• 危险类别码：
  R20/21/22
• WGK Germany：
  3
• 危险品运输编号：
  UN 3077 9/PG 3
• 储存条件：
  2-8°C

制备方法与用途

甲溴化异丙肾上腺素是一种口服活性的抗胆碱能毒蕈碱拮抗剂，能够抑制胃酸分泌，并常被用作治疗消化性溃疡的辅助药物。

文献信息

• Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
  申请人：Synergy Pharmaceuticals Inc.

  公开号：EP2527360A2

  公开（公告）日：2012-11-28

  The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition, including Crohn's disease and ulcerative colitis, and cancer.

  本发明提供了新型鸟苷酸环化酶-C激动剂肽及其在治疗人类疾病（包括胃肠道疾病、炎症或癌症（如胃肠道癌症））中的用途。这些肽既可单独施用，也可与 cGMP 依赖性磷酸二酯酶抑制剂联合施用。胃肠道疾病可分为肠易激综合征、便秘或胃酸过多等。胃肠道疾病可分为炎症性肠病或其他胃肠道疾病，包括克罗恩病、溃疡性结肠炎和癌症。
• Methods and compositions for the treatment of heart failure and other disorders
  申请人：Ironwood Pharmaceuticals, Inc.

  公开号：EP2650303A1

  公开（公告）日：2013-10-16

  Peptides that act as GC-C receptor agonists and contain at least one D-Cys and are useful for the treatment of diuresis and heart disease as well as other disorders are described.

  本文介绍了作为 GC-C 受体激动剂并含有至少一种 D-Cys 的多肽，这些多肽可用于治疗利尿和心脏病以及其他疾病。
• AGONISTS OF GUANYLATE CYCLASE USEFUL FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA
  申请人：Synergy Pharmaceuticals Inc.

  公开号：EP2923706A1

  公开（公告）日：2015-09-30

  This invention also provides a method to prevent, control and treat lipid metabolism disorder, a biliary disorder, cardiovascular disease, obesity or an endocrine disorder by administering at least one agonist of guanalyte cyclase receptor either alone or in combination with a compound typically used to treat the disorder and or with an inhibitor of cGMP-dependent phosphodieasterases.

  本发明还提供了一种预防、控制和治疗脂质代谢紊乱、胆道疾病、心血管疾病、肥胖症或内分泌紊乱的方法，其方法是单独或与通常用于治疗该疾病的化合物以及或与 cGMP 依赖性磷酸二酯酶抑制剂联合使用至少一种鸟苷酸环化酶受体激动剂。
• AGONISTS OF GUANYLATE CYCLASE USEFUL FOR THE TREATMENT OF COLON CANCER
  申请人：Synergy Pharmaceuticals Inc.

  公开号：EP3357502A1

  公开（公告）日：2018-08-08

  This invention also provides a method to prevent, control, and treat lipid metabolism disorder, a biliary disorder, cardiovascular disease, obesity or an endocrine disorder by administering at least one agonist of guanalyte cyclase receptor either alone or in combination with a compound typically used to treat the disorder and or with an inhibitor of cGMP-dependent phosphodieasterases.

  本发明还提供了一种预防、控制和治疗脂质代谢紊乱、胆道疾病、心血管疾病、肥胖症或内分泌紊乱的方法，其方法是单独使用至少一种鸟苷酸环化酶受体激动剂，或将其与通常用于治疗该紊乱的化合物和或与 cGMP 依赖性磷酸二酯酶抑制剂联合使用。
• Agonists of guanylate cyclase and their uses
  申请人：SYNERGY PHARMACEUTICALS, INC.

  公开号：US10118946B2

  公开（公告）日：2018-11-06

  This invention provides novel guanylate cyclase C (GC-C) agonists and their therapeutic use. The agonists may be used either alone or in combination with one or more additional agents.

  本发明提供了新型鸟苷酸环化酶 C (GC-C) 激动剂及其治疗用途。这些激动剂既可单独使用，也可与一种或多种其他药物联合使用。